Method for reducing malodor of chondroitin

ABSTRACT

The present invention relates to a method of removing or masking odor associated with chondroitin derived from marine life. The method comprises blending the chondroitin with citric acid, silicon dioxide, and optionally a flavorant to yield a substantially non-malodorous blend.

This application claims priority from provisional application No.60/274806. filed Mar. 9, 2001, and is a divisional application ofco-pending application Ser. No. 10/094,096.

FIELD OF THE INVENTION

The present invention relates to a method for the removal or masking ofmalodor from chondroitin derived from marine life. The present inventionalso relates to chondroitin compositions derived from marine life whichlack a malodor.

BACKGROUND OF THE INVENTION

Chondroitin and glucosamine are chondroprotective agents used for thetreatment of osteoarthritis and related diseases. Chondroitin sulfate isa soluble mucopolysaccharide derived from bovine, ovine or sharkcartilage. Chondroitin sulfate derived from marine life, such ascartilage isolated from sharks, provides a rich, pure, and readilyabsorbed source of chondroitin.

Chondroitin sulfate has been reported to be effective in tissue repairand cartilage regeneration. Combinations of glucosamine and chondroitinare also effective in cartilage regeneration and joint maintenance.Chondroitin and glucosamine appear to act by increasing chondrocyteanabolic activity and suppressing degradative action of mediators oncartilage. This appears to facilitate natural tissue repair. See, e.g.,H. Benedikt, Nat. Pharm., 1(8): 1, 22 (1997) and C. Bassleer, et al.,Int. J. Tiss. Reac. XIV(5): 231-241: (1992). Additionally, chondroitinand glucosamine are believed to be safer and less toxic than steroids ornon-steroidal anti-inflammatory drugs commonly administered to treatarthritis and related musculo-skeletal diseases.

Although shark cartilage is rich source of chondroitin, shark-derivedchondroitin has a strong malodor.

Therefore, there is a need for compositions containing shark-derivedchondroitin without its malodor and methods of preparing the same.Removal of the malodor associated with such chondroitin would improveconsumer acceptability and enhance patient compliance.

OBJECT OF THE INVENTION

It is an object of the invention to provide a method for removing and/orreducing the malodor associated with chondroitin derived from marinelife. It is further an object of the invention to provide chondroitinderived from marine life which exhibits reduced levels of malodornormally associated with such a composition.

SUMMARY OF THE INVENTION

The invention relates to a method of removing or masking odor associatedwith chondroitin sulfate. The method comprises blending the chondroitinwith citric acid, silicon dioxide, and, optionally a flavorant, to yielda substantially non-malodorous blend. The blend may be formed into asolid dosage form, such as a tablet.

Another embodiment of the invention is a composition comprisingchondroitin, citric acid, silicon dioxide, and an optional flavorant.

DETAILED DESCRIPTION OF THE INVENTION

The present inventors have discovered that the malodor associated withchondroitin derived from marine life may be removed or masked byblending the chondroitin with citric acid and silicon dioxide.Chondroitin compositions produced through the use of the presentinvention exhibit reduced levels of the malodor normally associated withsuch chondroitin compositions derived from marine sources

The chondroitin may be any chondroitin-containing composition. Commonlyavailable are two salts, namely chondroitin sulfate or chondroitinhydrochloride. Preferably, the chondroitin is the sulfate salt and isderived from shark cartilage. Most preferably, the chondroitin is watersoluble, such as Polychon 60/40 available from Vanson, Inc. (PfanstiehlLaboratory Inc.) of Waukegan, Ill.

The amount of citric acid in the composition broadly ranges from about0.05 to about 10% percent by weight based upon 100 percent by weight oftotal composition. Preferably, the amount of citric acid in thecomposition is about 1.5 percent by weight on the same basis.

The amount of silicon dioxide in the composition ranges broadly fromabout 0.01 to about 2.0 percent by weight based upon 100 percent byweight of total composition. Preferably, the amount of silicon dioxidein the composition is preferably about 0.2 percent by weight on the samebasis.

Other adjuvants as known to those in the art, such as disintegrants,antioxidants, lubricants and binders, may be included in thecomposition.

Optionally, the composition may contain a flavorant. The flavorant maybe a natural flavorant, an artificial flavorant, or a combinationthereof. Preferred flavorants include, but are not limited to, naturallemon extract, artificial lemon extract, 10 natural orange extract, andany combination of any of the foregoing. The composition may contain anamount of flavorant effective in masking any degree of malodor remainingin the chondroitin-containing composition. The amount of flavorant inthe composition broadly ranges from 0.0 to about 10 percent by weightbased upon 100 percent by weight of total composition. Preferably, theflavorant is present in the composition in an amount of about 3.3percent by weight on the same basis.

Combinations of chondroitin and glucosamine compounds are popular.Therefore, glucosamine or a salt thereof, may also be included in thecomposition. Preferred salts of glucosamine indude, but are not limitedto, glucosamine hydrochloride and glucosamine sulfate. The weight ratioof chondroitin sulfate to glucosamine generally ranges from about 1:100to about 100:1. The typical mixture found in the composition which arecurrently commercialized have a weight ratio of about 5:4. Therefore,the preferred weight ratio of glucosamine to chondroitin is about 5:4. Apreferred glucosamine is glucosamine hydrochloride, such as thatproduced by Wilke International of 15036 W. 106^(th) Street, Lexexa,Kans. 66215.

The composition may be incorporated into or formed into solid dosageforms, such as capsules or tablets.

The claimed composition may be prepared by blending the chondroitincompound with citric acid, silicon dioxide, and optionally a flavorant.Preferably, citric acid, silicon dioxide, and the flavorant are mixed toform a citric acid/silicon dioxide/flavorant mixture prior to blendingwith the chondroitin sulfate. The citric acid/silicon dioxide/flavorantmixture is preferably prepared by mixing silicon dioxide and theflavorant and then adding citric acid.

EXAMPLE

The following example illustrates the invention without limitations. Allamounts are by weight unless otherwise specified.

Example 1

Silicon dioxide (3.0 mg) available as Aerosil from Degussa-HulsCorporation of Ridgefield Park, N.J. was blended with 49.5 mg of naturallemon extract for about 3 minutes in a PK blender (manufactured byPatterson & Keely, a divison of Harsco Corporation, East Stroudsburg,Pa. 18301). Citric acid (22.5 mg) was added to the silicon dioxide/lemonextract blend and blended for about 2 minutes.

A 5:4 mixture of glucosamine sulfate and chondroitin sulfate wasprepared by mixing in a mixing bowl with a PK Blender 750 grams ofglucosamine hydrochloride (marketed by Pfanstiehl Laboratory Inc. of1219 Glen Rock Avenue, Waukegan, Ill. 60085) and 600 grams ofchondroitin sulfate (marketed under the tradename Polychon® 60/40 byVanson, Inc. of Waukegan, Ill.). The mixture was placed into the feedhopper of a Fitzpatric IR-520 Chilsonator. The chilsonator converted themixture into a compacted solid. The chilsonator was operated at a rollspeed of 6 rpm, roll pressure of 1250 psig, vertical screw speed of 150rpm, and horizontal screw speed of 15 rpm. The compacted product formedin the chilsonator was passed through a Fitzpatric M5A mill and thegranulated product collected. The mill was operated at a rotor speed of300 rpm with a 4 bar rotor and a 0.050 inch rasping screen. The relativehumidity was 57% and the temperature was 75° F.

The chondroitin sulfate/glucosamine hydrochloride mixture, 30.0 mg ofsodium starch glycolate, and 15.0 mg of magnesium stearate were added tothe silicon dioxide/lemon extract/citric acid blend and blended forabout 3 minutes. The resulting powder blend was then compressed into atablet at a suitable compression pressure using a rotary tablet pressand standard tooling. The resulting tablet did not exhibit any malodor,differing substantially from that exhibited by the initial chondroitinsulfate component.

Many variations of the present invention will suggest themselves tothose skilled in the art in light of the above, detailed description.All such obvious variations are within the full intended scope of theappended claims.

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 15. Acomposition exhibiting reduced malodor comprising a. chondroitin derivedfrom marine life; b. citric acid, and c. silicon dioxide.
 16. Thecomposition of claim 15, wherein said chondroitin is chondroitinsulfate.
 17. The composition of claim 15, wherein said chondroitin ischondroitin sulfate derived from shark cartilage.
 18. The composition ofclaim 15, wherein the amount of citric acid ranges from about 0.5 toabout 10 percent by weight based upon 100 percent by weight of thecomposition.
 19. The composition of claim 16, wherein the amount ofcitric acid is about 1.5 percent by weight, based upon 100 percent byweight of the composition.
 20. The composition of claim 15, wherein theamount of said silicon dioxide ranges from about 0.01 to about 2.0percent by weight, based upon 100 percent by weight of the composition.21. The composition of claim 6, wherein the amount of said silicondioxide is about 0.2 percent by weight, based upon 100 percent by weightof the composition.
 22. The composition of claim 15 further comprising aflavorant.
 23. The composition of claim 22 wherein said flavorant isselected from the group consisting of natural flavorants, artificialflavorants, or a combination thereof.
 24. The composition of claim 22wherein the flavorant is present in amount up to about 10 percent byweight, based upon 100 percent by weight of the composition.
 25. Thecomposition claim 22 wherein the flavorant is present in an amount ofabout 3.3 percent by weight, based upon 100 percent by weight of thecomposition.
 26. The composition of claim 15 further comprisingglucosamine or a salt thereof.
 27. A composition of 26, wherein theweight ratio of glucosamine or salt thereof to chondroitin is about 5:4.28. A solid dosage form comprising the composition of claim
 15. 29. Acomposition which does not exhibit malodor comprising chondroitinsulfate derived from marine life.
 30. The composition of claim 29wherein said chondroitin is derived from shark cartilage.